3＇-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethyl- ation of azithromycin, i. e. , azithromycin loses a methyl group on the 3＇-N position. In this study, bulk product was purifi...3＇-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethyl- ation of azithromycin, i. e. , azithromycin loses a methyl group on the 3＇-N position. In this study, bulk product was purified with chromatographic separation. It was observed that 3＇-N-demethylaz- ithromycin was also a precursor of other impurities. Simultaneously, another derivative was synthe- sized, i. e. , 3＇-N-demethyl-3＇-N-formylazithromycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of de- rivatives were identified by 1H-NMR and MS.展开更多
基金Supported by the Major Projects of National Science & Technology(2009ZX09313-027)
文摘3＇-N-demethylazithromycin is an impurity in azithromycin drug. It is derived by demethyl- ation of azithromycin, i. e. , azithromycin loses a methyl group on the 3＇-N position. In this study, bulk product was purified with chromatographic separation. It was observed that 3＇-N-demethylaz- ithromycin was also a precursor of other impurities. Simultaneously, another derivative was synthe- sized, i. e. , 3＇-N-demethyl-3＇-N-formylazithromycin. Reaction conditions were optimized with the HPLC method and good-quality and high-yield derivative product was achieved. The structures of de- rivatives were identified by 1H-NMR and MS.
